SML2756
Bremelanotide acetate
≥98% (HPLC)
Synonym(s):
Ac-Nle-Asp-His-D-Phe-Arg-Trp-Lys (Asp-Lys), acetate salt, Acetyl-[Nle4, Asp5, D-Phe7, Lys10]-cyclo-α-melanocyte, PT 141 acetate, PT-141 acetate, PT141 acetate
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About This Item
Empirical Formula (Hill Notation):
C50H68N14O10 · xC2H4O2
CAS Number:
Molecular Weight:
1025.16 (free base basis)
UNSPSC Code:
12352200
NACRES:
NA.77
Quality Level
Assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to off-white
shipped in
wet ice
storage temp.
−20°C
Biochem/physiol Actions
Bremelanotide (PT-141) is a brain-penetrant, alpha-melanocyte-stimulating hormone (α-MSH)-derived cyclic heptapeptide agonist toward melanocortin receptors, including MC1R, MC3R and MC4R (affinty = 10 nM by competitive binding against 0.2 nM NDP-α-MSH using human MC4R-expressing HEK-293). Bremelanotide induces cAMP accumulation in hMC4R-expressing HEK-293 cells and exhibits in vivo sexual arousal efficacy among both male (50 μg/kg intranasally or 50-500 pg/kg via lateral ventricle injection) and female rats (100-200 μg/kg sc or 800 μg/kg via lateral ventricle injection) by activating neurons in brain regions responsible for sexual function.
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
监管及禁止进口产品
Certificates of Analysis (COA)
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K L Aughton et al.
British journal of pharmacology, 155(2), 236-243 (2008-07-01)
Hypothalamic neuropeptides centrally modulate sexual arousal. However, the role of neuropeptides in peripheral arousal has been ignored. Vascular and non-vascular smooth muscle relaxation in the vagina is important for female sexual arousal. To date, in vitro studies have focused on
P B Molinoff et al.
Annals of the New York Academy of Sciences, 994, 96-102 (2003-07-10)
PT-141, a synthetic peptide analogue of alpha-MSH, is an agonist at melanocortin receptors including the MC3R and MC4R, which are expressed primarily in the central nervous system. Administration of PT-141 to rats and nonhuman primates results in penile erections. Systemic
James Pfaus et al.
The journal of sexual medicine, 4 Suppl 4, 269-279 (2007-11-21)
Bremelanotide is an analogue of the naturally occurring peptide alpha-melanocyte-stimulating hormone (alpha-MSH). It stimulates erection in men and male rats, and is currently in clinical trials for the treatment of erectile dysfunction. To review the effects of bremelanotide, an analogue
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